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ChEMBL ligand: CHEMBL1292 (Chlofazimine, Clofazimine, Clofaziminum, Colfazimine, G 30320, G-30320, Lamprene, NSC-141046) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
ChEMBL | TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) | F | 4.54 | pIC50 | 28700 | nM | IC50 | Pharm Res (2003) 20: 537-544 [PMID:12739759] |
Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779] | ||||||||
ChEMBL | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100 | B | 4.4 | pIC50 | 40000 | nM | IC50 | J Med Chem (2010) 53: 4259-4265 [PMID:20426472] |
ChEMBL | Inhibition of Trypanosoma cruzi cruzaine in presence of 0.01% Triton | B | 4.4 | pIC50 | 40000 | nM | IC50 | Eur J Med Chem (2015) 93: 338-348 [PMID:25707014] |
ChEMBL | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2010) 53: 4259-4265 [PMID:20426472] |
ChEMBL | Inhibition of Trypanosoma cruzi cruzaine in absence of 0.01% Triton | B | 5.22 | pIC50 | 6000 | nM | IC50 | Eur J Med Chem (2015) 93: 338-348 [PMID:25707014] |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells | F | 5.96 | pIC50 | 1100 | nM | IC50 | Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514] |
ChEMBL | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells | F | 6 | pIC50 | 1000 | nM | IC50 | Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514] |
ChEMBL | TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells | F | 6.22 | pIC50 | 600 | nM | IC50 | Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite growth after 72 hrs by parasite lactate dehydrogenase assay | F | 5.15 | pIC50 | 7020 | nM | IC50 | Bioorg Med Chem (2015) 23: 55-65 [PMID:25497962] |
ChEMBL | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 assessed as inhibition of parasite growth after 72 hrs by parasite lactate dehydrogenase assay | F | 5.32 | pIC50 | 4820 | nM | IC50 | Bioorg Med Chem (2015) 23: 55-65 [PMID:25497962] |
ChEMBL | DNDI: Malaria in Vitro, 72 hour | F | 5.39 | pIC50 | 4100 | nM | IC50 | Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]